title: Purgative components in rhubarbs: adrenergic receptor inhibitors linked with glucose carriers.
abstract: Rhubarbs and their extractives have been used as cathartic for many years. There have been numerous breakthroughs in the pharmacological research of the drug. However, as the key point of the mechanism, the targets of the effective components still remain unclear. In this paper, with an in vitro system of isolated intestine, we found that both the rhubarb extractives and the anthraquinone derivatives can antagonize the adrenaline effectively. Furthermore, computer based docking provided the binding model of the anthraquinone derivatives and adrenergic receptor. Then, based on the results of the small intestinal promotion and purgative effect experiments in vivo, we built an "inhibitor-carrier" hypothesis to elucidate the mechanism of rhubarb. This work provided key massages for the pharmacological research of rhubarb, such a common and active medicinal plant, and might be of help for the development of new purgative drugs.
authors.affiliation: MOE Key Laboratory of Protein Sciences, Laboratory of Molecular Pharmacology and Pharmaceutical Sciences, School of Medicine and School of Life Sciences, Tsinghua University, Beijing 100084, China.
authors.forename: Tian-Shi
authors.initials: TS
authors.lastname: Feng
authors.affiliation: MOE Key Laboratory of Protein Sciences, Laboratory of Molecular Pharmacology and Pharmaceutical Sciences, School of Medicine and School of Life Sciences, Tsinghua University, Beijing 100084, China.
authors.forename: Zhi-Yi
authors.initials: ZY
authors.lastname: Yuan
authors.affiliation: MOE Key Laboratory of Protein Sciences, Laboratory of Molecular Pharmacology and Pharmaceutical Sciences, School of Medicine and School of Life Sciences, Tsinghua University, Beijing 100084, China.
authors.forename: Run-Qing
authors.initials: RQ
authors.lastname: Yang
authors.affiliation: MOE Key Laboratory of Protein Sciences, Laboratory of Molecular Pharmacology and Pharmaceutical Sciences, School of Medicine and School of Life Sciences, Tsinghua University, Beijing 100084, China.
authors.forename: Shuang
authors.initials: S
authors.lastname: Zhao
authors.affiliation: MOE Key Laboratory of Protein Sciences, Laboratory of Molecular Pharmacology and Pharmaceutical Sciences, School of Medicine and School of Life Sciences, Tsinghua University, Beijing 100084, China.
authors.forename: Fan
authors.initials: F
authors.lastname: Lei
authors.affiliation: National Institutes for Food and Drug Control, Beijing 100050, China.
authors.forename: Xin-Yue
authors.initials: XY
authors.lastname: Xiao
authors.affiliation: MOE Key Laboratory of Protein Sciences, Laboratory of Molecular Pharmacology and Pharmaceutical Sciences, School of Medicine and School of Life Sciences, Tsinghua University, Beijing 100084, China.
authors.forename: Dong-Ming
authors.initials: DM
authors.lastname: Xing
authors.affiliation: Drug Discovery Facility, School of Life Sciences, Tsinghua University, Beijing 100084, China.
authors.forename: Wei-Hua
authors.initials: WH
authors.lastname: Wang
authors.affiliation: Drug Discovery Facility, School of Life Sciences, Tsinghua University, Beijing 100084, China.
authors.forename: Yi
authors.initials: Y
authors.lastname: Ding
authors.affiliation: MOE Key Laboratory of Protein Sciences, Laboratory of Molecular Pharmacology and Pharmaceutical Sciences, School of Medicine and School of Life Sciences, Tsinghua University, Beijing 100084, China. Electronic address: lijundu@mail.tsinghua.edu.cn.
authors.forename: Li-Jun
authors.initials: LJ
authors.lastname: Du
mesh_terms: D018674:Adrenergic Antagonists / Q000494:pharmacology*; D000880:Anthraquinones / Q000494:pharmacology*; D002400:Cathartics / Q000494:pharmacology*; D004337:Drug Carriers; D004365:Drugs, Chinese Herbal / Q000494:pharmacology*; D005947:Glucose; D007413:Intestinal Mucosa / Q000378:metabolism; D007422:Intestines / Q000187:drug effects*; D011941:Receptors, Adrenergic / Q000378:metabolism*; D012250:Rheum / Q000737:chemistry*
chemical_list: D018674:Adrenergic Antagonists; D000880:Anthraquinones; D002400:Cathartics; D004337:Drug Carriers; D004365:Drugs, Chinese Herbal; D011941:Receptors, Adrenergic; D005947:Glucose
keywords: Aloe-emodin (PubChem CID: 10207); Chrysophanol (PubChem CID: 10208); Emodin (PubChem CID: 3220); Large intestines; Physcione (PubChem CID: 10639); Rhein (PubChem CID: 10168); Rhubarb; Small intestines; β-Adrenal receptor